Abstract
Activity-guided fractionation of a MeOH extract of the roots of Saussurea lappa C.B.Clarke (Compositae), using an in vitro protein tyrosine phosphatase 1B (PTP1B) inhibition assay, led to the isolation of four active constituents: betulinic acid (1), betulinic acid methyl ester (2), mokko lactone (3) and dehydrocostuslactone (4), along with nine inactive compounds. Our findings indicate that betulinic acid (1) and its methyl ester 2, as well as the two guaiane sesquiterpenoids 3 and 4 are potential lead moieties for the development of new PTP1B inhibitors.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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4-Butyrolactone / analogs & derivatives
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4-Butyrolactone / chemistry
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4-Butyrolactone / isolation & purification
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4-Butyrolactone / pharmacology
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Betulinic Acid
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Enzyme Inhibitors / chemistry*
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Enzyme Inhibitors / isolation & purification
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Enzyme Inhibitors / pharmacology
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Humans
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Lactones / chemistry
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Lactones / isolation & purification
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Lactones / pharmacology
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Pentacyclic Triterpenes
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Plant Roots / chemistry
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Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
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Saussurea / chemistry*
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Sesquiterpenes / chemistry
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Sesquiterpenes / isolation & purification
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Sesquiterpenes / pharmacology
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Sesquiterpenes, Guaiane / chemistry*
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Sesquiterpenes, Guaiane / isolation & purification
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Sesquiterpenes, Guaiane / pharmacology
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Triterpenes / chemistry*
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Triterpenes / isolation & purification
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Triterpenes / pharmacology
Substances
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Enzyme Inhibitors
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Lactones
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Pentacyclic Triterpenes
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Sesquiterpenes
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Sesquiterpenes, Guaiane
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Triterpenes
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betulinic acid methyl ester
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mokko lactone
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dehydrocostus lactone
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Protein Tyrosine Phosphatase, Non-Receptor Type 1
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4-Butyrolactone
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Betulinic Acid